Omeprazole is a commonly prescribed drug for patients with peptic ulcerations. Its main mechanism of action is related to inhibition of H(+)-K(+)-ATP-ase, albeit it may also block carbonic anhydrase. This study evaluates the effects of acute and prolonged (3- or 7-day) intragastrical administration of omeprazole on the anticonvulsant activity of carbamazepine or diphenylhydantoin against maxima...

4(3H)-Quinazolinones 1 are known for more than a century [1]. Molecules based on quinazoline and quinazolinone exhibit a multitude of interesting pharmacological activities [2], including anticonvulsant, antibacterial and antidiabetic activity [3,4]. The important natural and synthetic 4(3H)-quinazolinones include l-vasicinone 2 [5], chrysogine 3 [6], methaquinalon 4 [7] – a sedative, piriqualo...

methyl indole derivative of some 6-aryl-4,5-dihydropyridazin-3(2h)-ones (3a-e) were synthesized by mannich reaction and evaluated as anticonvulsant against mes (50ma, for 2sec), inh (250mg/kg), scptz (80mg/kg) and str (3mg/kg) induced convulsion methods at 50 mg/kg dose level. all compounds 3a-e were also evaluated as antitubercular agent against m. tuberculosis h37rv by maba method. all compou...

Anticonvulsant potential and neurotoxicity of certain new imidazole-containing arylsemicarbazones 6a-p are reported. The test compounds 6a-p exhibited anticonvulsant activity mainly in the scPTZ screen. Compound 6p emerged as the most active surrogate displaying 100% protection at a dose level of 636 μ mol/kg in the scPTZ screen without any neurotoxicity. The assigned (E)-configuration of the t...

Several heteroaryl semicarbazones were prepared by the reaction of heteroaryl hydrazine carboxamide with aryl aldehydes or ketones. The structures of the synthesized compounds were confirmed by spectral data and elemental analyses. Compounds were tested for anticonvulsant activity utilizing pentylenetetrazole-induced seizure (PTZ) and maximal electroshock seizure (MES) tests at 30, 100 and 300 ...

Benzodiazepines are useful drugs for treatment of sleep disorders, anxiety, seizure cases and skeletal muscle cramps. Some derivatives of 2-(2-Phenoxy) phenyl-1, 3, 4-oxadiazole were synthesized as benzodiazepine receptor agonists. Conformational analysis and superimposition of energy minima conformers of the compounds on estazolam, a known benzodiazepine agonist, reveal that the main proposed ...

OBJECTIVE The mammalian target of rapamycin (mTOR) pathway integrates signals from different nutrient sources, including amino acids and glucose. Compounds that inhibit mTOR kinase activity such as rapamycin and everolimus can suppress seizures in some chronic animal models and in patients with tuberous sclerosis. However, it is not known whether mTOR inhibitors exert acute anticonvulsant effec...

Previously obtained picolinic acid benzylamide is a potent anticonvulsant with low neurotoxicity. In search for new effective anticonvulsants twelve new benzylamides (1-12) were synthesized and preliminary evaluated in the Anticonvulsant Screening Program (ASP) of Antiepileptic Drug Development Program (ADDP) of NIH. Two of them appeared the most promising: 1-cyclopentenecarboxylic acid benzyla...

the role of cu, zn and co in human physiology is well documented. isatin and glycine have inhibitory effects on central nervous system. to capitalize on these features metal complexes of isatin-3-glycine were prepared and evaluated for anticonvulsant activity. the cu (ii) complex was found to be most active among the compounds. the compounds were screened against staphylococcus aureus, escheric...